Abstract:
Cancer is the second leading cause of death in South Africa. The
critical role that microtubules play in cell division makes them an ideal target
for the development of chemotherapeutic drugs that prevent the
hyperproliferation of cancer cells. The new in silico-designed estradiol
analogue 2-ethyl-3-O-sulfamoyl-estra-1,3,5(10)16-tetraene (ESE-16) was
investigated in terms of its in vitro antiproliferative effects on the esophageal
carcinoma SNO cell line at a concentration of 0.18 μM and an exposure
time of 24 h. Polarization-optical differential interference contrast and
triple fluorescent staining (propidium iodide, Hoechst 33342 and acridine
orange) revealed a decrease in cell density, metaphase arrest, and the
occurrence of apoptotic bodies in the ESE-16-treated cells when compared to
relevant controls. Treated cells also showed an increase in the presence of
acidic vacuoles and lysosomes, suggesting the occurrence of
